| 寄立 麻琴（よりたて まこと） | データ更新日：2023.06.21 |
助教 ／
薬学研究院
創薬科学部門
薬物分子設計学分野
| 1. | 寄立麻琴, 天然変性タンパク質をターゲットとした位置選択的タンパク質修飾法とADCの開発, BIO Clinica, 2021.06, 近年多くの薬物抗体複合体(Antibody Drug Conjugate: ADC)が臨床試験に上がっているが， その不均一性による品質の担保が問題となっ ている。本問題の解決には，ADC を合成する 段階で均一な結合サイトに均一な個数の薬物 を導入することが必要不可欠である。しかし， 多数の反応性官能基が共存するタンパク質の 一部のアミノ酸を選択的に変換することは容 易ではない。本稿では，天然タンパク質中に 多く含まれる Tyr および Lys 残基の位置選択 的な化学修飾法について述べる。. |
| 2. | Makoto Yoritate, Quinonemethide in Chemical Biology, Journal of Synthetic Organic Chemistry, Japan, 10.5059/yukigoseikyokaishi.78.728, 2020.07, [URL], Quinonemethides(QM)are reactive chemical species which can be generated from o─ and p─hydroxy benzyl alcohol derivatives even in aqueous media. Its unique reactivity is frequently utilized in organic synthesis and chemical biology. The high electrophilicity of QM would result in the rapid formation of a covalent bond with nucleophilic amino─acid residues in peptide or nucleic─acid bases. In addition, released leaving groups in the formation of QM can be designed as, for example, bioactive molecules for drug─delivery system and fluorophores for activity─based probe. Herein, recent reports associated with the quinonemethide chemistry are described.. |
| 3. | Takaaki Sato, Makoto Yoritate, Hayato Tajima, Noritaka Chida, Total synthesis of complex alkaloids by nucleophilic addition to amides, Organic and Biomolecular Chemistry, 10.1039/c8ob00733k, 2018.01, [URL], Nucleophilic addition to amides has been recognized as a promising transformation for total synthesis of complex alkaloids. Amides can accept two different organometallic reagents through the nucleophilic addition, which enables it to serve as a stable surrogate of multi-substituted amines. However, the nucleophilic addition has been overlooked for a long time due to three main reasons: low electrophilicity of amide carbonyls, potential hydrolysis of the reaction intermediate and excess addition of an organometallic reagent. This mini review focuses on the recent progress of total synthesis of complex alkaloids based on the nucleophilic additions to N-alkoxyamides, tertiary amides and secondary amides.. |
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